Cholinergic Agonists & Antagonists

Bethanechol

Cholinergic Agonist

MOA: muscarinic agonist at receptor in the bladder

Primary indication: treats urinary retention

Side effects: cholinergic side effects (parasympathetic)

Pilocarpine

Cholinergic Agonist

MOA: Muscarinic agonist at muscarinic receptor in the eye and salivary glands

Primary indication: treats glaucoma and dry mouth

Side effects: cholinergic side effects (parasympathetic)

Edrophonium

Cholinergic Agonist

MOA: AChEi that acts primarily on skeletal muscle

Primary indication: treats myasthenia gravis (also used as diagnostic test for this disease); reversal agent for non-depolarizing neuromuscular blockers

Side effects: cholinergic side effects when given in excess (too much ACh around)

Pralidoxime

Cholinergic Agonist

MOA: Reactivates cholinesterase (does this in case of
organophosphate poisoning by breaking AChE bond with the organophosphate molecule) 

Primary indication: treat organophosphate poisoning

Donepezil

Cholinergic Agonist

MOA: AChEi that acts primarily in the CNS

Primary indication: treats Alzheimer’s

Side effects: Cholinergic side effects (parasympathetic)

Atropine

Cholinergic Antagonist

MOA: Muscarinic antagonist at muscarinic receptors in the heart; also acts at other target organs as treatment of symptoms of organophosphate poisoning (where there’s too much ACh around)

Primary indication: treats bradycardia; treats parasympathetic symptoms of organophosphate poisoning

Side effects: Anticholinergic side effects (sympathetic)

Hycosamine

Cholinergic Antagonist

MOA: Muscarinic antagonist at muscarinic receptors stomach and lungs

Primary indication: reduces bronchial and pharyngeal secretions; reduces HCl production to treat PUD

Side effects: Anticholinergic side effects (sympathetic)

Scopolamine

Cholinergic Antagonist

MOA: Muscarinic antagonist at muscarinic receptors in salivary glands and bronchials

Primary indicaiton: treats motion sickness and drooling (prevents excessive salivation) 

Side effects: Anticholinergic side effects (sympathetic); typically given as a patch formulation

Glycopyrrolate

Cholinergic Antagonist

MOA: Muscarinic antagonist at muscarinic receptors in salivary glands

Primary indication: treats drooling (prevents excessive salivation)

Side effects: Anticholinergic side effects (sympathetic)

Ipratropium

Cholinergic Antagonist

MOA: Muscarinic antagonist at muscarinic receptors in the lungs

Primary indication: treat wheezing from Asthma/COPD

Side effects: Anticholinergic side effects (sympathetic)

Oxybutynin

Cholinergic Antagonist

MOA: Muscarinic antagonist at muscarinic receptors in the bladder

Primary indication: treat urinary incontinence/overactive bladder

Side effects: Anticholinergic side effects (sympathetic)

Pancronium and Cistracurium

Cholinergic Antagonist

MOA: Non-depolarizing neuromuscular blocker (competitive antagonist at nicotinic receptors)

Primary indication: skeletal muscle relaxation during surgery or mechanical ventilation

Side effects: Can be reversed by AChEi

Succinylcholine

Cholinergic Antagonist

MOA: Depolarizing neuromuscular blocker at nicotinic receptors (it is technically an agonist b/c it attaches the ACh receptor causing

depolarization. However, the EFFECT of persistent depolarization is paralysis of the skeletal muscle

Primary indication: Skeletal muscle relaxation during surgery or mechanical ventilation

Side effects: Cannot be reversed by AChEi